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Fasudil and Vardenafil compound preparation and preparation method thereof

A technology of fasudil and vardenafil, applied in the field of pharmacy, can solve problems such as complicated treatment and unsatisfactory effects

Active Publication Date: 2011-09-14
TIANJIN CHASE SUN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Pulmonary arterial hypertension is common in young patients and is an extremely nasty disease whose treatment is complicated and the effect is not ideal

Method used

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  • Fasudil and Vardenafil compound preparation and preparation method thereof
  • Fasudil and Vardenafil compound preparation and preparation method thereof
  • Fasudil and Vardenafil compound preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075]

[0076]

[0077] Preparation:

[0078] After crushing the prescribed amount of fasudil and vardenafil through a 120-mesh sieve, mix them evenly with low-substituted hydroxypropyl cellulose, lactose, microcrystalline cellulose, starch, and calcium hydrogen phosphate that have passed through an 80-mesh sieve to obtain a mixed powder , add 10% starch slurry to make soft material, pass through 24 mesh sieve to granulate, ventilate and dry at 55°C, after 20 mesh sieve granulation, mix with magnesium stearate evenly, compress into tablets to obtain compound tablet core.

Embodiment 2

[0080]

[0081] Preparation:

[0082] Grind the prescribed amount of Fasudil through a 100-mesh sieve, mix evenly with low-substituted hydroxypropyl cellulose, lactose, and microcrystalline cellulose that have passed through an 80-mesh sieve, and add 2% hydroxypropyl methylcellulose as a soft material , granulated through a 24-mesh sieve, ventilated and dried at 55°C, granulated through a 20-mesh sieve and mixed evenly with magnesium stearate to obtain Granule 1 for later use.

[0083] Crush vardenafil in the prescribed amount through a 100-mesh sieve, mix evenly with low-substituted hydroxypropyl cellulose, lactose starch, and microcrystalline cellulose that have passed through an 80-mesh sieve, add 2% hydroxypropyl methylcellulose to make soft material, granulated through a 24-mesh sieve, ventilated and dried at 55°C, granulated through a 20-mesh sieve and mixed evenly with magnesium stearate to obtain granules 2 for later use.

[0084] The granule 1 and the granule 2 ar...

Embodiment 3

[0089]

[0090] Preparation:

[0091] Grind the prescribed amount of fasudil and vardenafil respectively through a 100-mesh sieve, pass through a 80-mesh sieve for lactose, starch, and low-substituted hydroxypropyl cellulose, and pass through a 60-mesh sieve for sodium lauryl sulfate and magnesium stearate ; Vardenafil and lactose are multiplied and mixed evenly, then mixed with fasudil, starch, sodium lauryl sulfate, magnesium stearate, low-substituted hydroxypropyl cellulose, filled with 3# capsules, Get compound capsules.

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PUM

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Abstract

The invention belongs to the field of pharmacy and relates to a Fasudil and Vardenafil compound preparation and a preparation method thereof. The Fasudil and Vardenafil compound preparation is used for treating pulmonary hypertension. The Fasudil and Vardenafil compound preparation comprises Fasudil, Vardenafil and pharmaceutically acceptable auxiliary materials such as skeleton materials and the like in a disintegrating agent, an adhesive, an excipient, a diluent, a lubricant and a sustained release preparation, wherein suitable carriers can be selected according to different formulations.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a compound preparation of fasudil and vardenafil and a preparation method thereof, which are used for the treatment of pulmonary hypertension. Background technique [0002] Fasudil [hexahydro-1-(5-isoquinolinesulfonyl)-homopiperazine, Fasudil] is a Rho kinase inhibitor. Its molecular weight is 327.83 and its molecular formula is C 14 h 17 N 30 2S·HCl, structural formula: [0003] [0004] Studies have confirmed that the Rho kinase pathway is one of the important pathogenic pathways leading to pulmonary artery constriction and pulmonary vascular remodeling in patients with pulmonary arterial hypertension. For pulmonary hypertension, fasudil can reduce the activity of Rho kinase, inhibit the contraction of pulmonary artery vascular smooth muscle, dilate pulmonary arteries, reduce pulmonary artery resistance, and reduce pulmonary arterial pressure. [0005] Vardenafil (Vardenafil) is t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/551A61K31/53A61K9/20A61K9/16A61P11/00A61P9/12
Inventor 姚小青孙长海董凯韩志东
Owner TIANJIN CHASE SUN PHARM CO LTD
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